Synthesis and rheological activity of new 1,2,4-triazole derivatives

Клен, Е. Э.; Халиуллин, Ф. А.; Spasov, A. A.; Makarova, N. N.; Багаутдинова, Л. Ф.; Науменко, Л. В.

doi:10.1007/s11094-009-0171-9

Cited by 5 publications

(2 citation statements)

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“…Учитывая, что лекарственные средства, созданные на основе комбинации веществ с известной фармакологической активностью и новых химических структур, могут приобретать более выраженную фармакологическую активность или проявлять совершенно иные биологические свойства, поиск в их ряду новых молекул-кандидатов в лекарства теоретически оправдан [29]. Это было подтверждено исследованиями, выполненными в БГМУ: установлено, что тиетан-содержащие гетероциклические соединения обладают гипотензивной [30], противовоспалительной [31], иммунотропной [32], гипогликемической [33], гемореологической [34], антиагрегационной [35], антиоксидантной [36], гепатопротективной активностью [37,38].…”

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Prospects for the creation of new drug candidates with antidepressant activity among thietanes

Nikitina,

Gaisina,

Klen

et al. 2023

Kazan Med J

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The article presents the results of systematic studies on the search for new biologically active molecules with antidepressant activity in the series of thietane-containing heterocyclic compounds and 3-substituted thietane dioxides. The used strategy for the search for antidepressant substances, based on in vivo pharmacological screening in combination with in silico methods of mathematical modeling and toxico-pharmacokinetic evaluation, is described. Studies of the biological activity of thietane-containing reaction products of azoles with thiiranes have been carried out in the series of thietanylimidazoles, titanixanthines, thietanyltriazoles, thietanyltriazolones, and 3-substituted thietane-1,1-dioxides (more than 300 compounds have been studied). The main results of the preclinical evaluation of promising drug candidates with antidepressant activity, 3-methoxythiethane-1,1-dioxide and 3-ethoxythiethane-1,1-dioxide, are presented. Both 3-substituted thietane-1,1-dioxides are characterized by low toxicity when administered intraperitoneally to mice (class IV low toxicity), the absence of toxic risks (mutagenic, carcinogenic, reproductive toxicity, local irritant action), high pharmaceutical potential (compliance with the rule of five Lipinsky), a wide range of action and pronounced antidepressant activity, not inferior to the reference drug amitriptyline (10 mg/kg), confirmed in highly valid in vivo models of depressive-like states (chronic mild stress and resident intruder). In tests of neuropharmacological interaction, it was found that the proposed mechanism of action of 3-substituted thietane-1,1-dioxides is associated with stimulation of 5-HT1A receptors, blockade of 5-HT2A/2C receptors and/or 2-adrenergic receptors. The need for further research is substantiated in order to create domestic first in class antidepressants on their basis.

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Prospects for the creation of new drug candidates with antidepressant activity among thietanes

Nikitina,

Gaisina,

Klen

et al. 2023

Kazan Med J

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“…Антиагрегаційна дія. В роботі [29] наведено оцінку реологічних властивостей похідних 1,2,4-триазолу, встановлено, що деякі з синтезованих сполук виявляють антиагрегаційну активність щодо еритроцитів порівняно з дією пентоксифіліну.…”

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Biological activity of the derivatives of 1,2,4-triazole

Kravchenko

Панасенко

Knysh

2018

Farm Zh

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The rapid development of modern medicine and pharmacy leads to an increase in synthetic drugs. Thus, in the professional literature says that one of the perspective directions are searching for new biologically active compounds including heterocyclic systems and the introduction of the latest in medical, pharmaceutical or veterinary practice. It is known that heterocyclic ring system 1,2,4-triazole moiety is promising for the synthesis of new active ingredients with various kinds of pharmacological actions. The aim of the study was the analysis of literature and patent sources over the past 10 years and the generalization of the results for certain types of biological activity of 1,2,4-triazole. Results of literary analysis show a wide range of biological activity of 1,2,4-triazole-3-tion. The data determine the relevance of further research of derivatives of 1,2,4-triazole in the actoprotective, antimicrobial, antifungal, antihypoxic, hypoglycemic, analgesic, antiinflammatory and others activity in order to find new highly effective in terms of biological substances that can form the basis of new medicines.

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